2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. Fadrozole

Fadrozole  (Synonyms: CGS 16949A free base; (Rac)-FAD286)

Cat. No.: HY-14247A Purity: 99.69%
COA Handling Instructions

Fadrozole (CGS 16949A free base) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.

For research use only. We do not sell to patients.

Fadrozole Chemical Structure

Fadrozole Chemical Structure

CAS No. : 102676-47-1

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10 mM * 1 mL in DMSO USD 61 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Fadrozole:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Fadrozole

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 CYP19 CYP26 CYP51

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Fadrozole (CGS 16949A free base) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.

IC50 & Target

Aromatase

 

In Vitro

Fadrozole hydrochloride is a very potent inhibitor of both human placental and rat ovarian aromatase. In hamster ovarian slices, fadrozole hydrochloride inhibits the production of estrogen with an IC50 of 0.03 μM. The production of progesterone is inhibited with an IC50 of 120 μM. Synthesis of other cytochrome P-450 dependent steroids can be suppressed to various degrees with higher doses of fadrozole hydrochloride. [1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

Fadrozole hydrochloride is able to inhibit the aromatase-mediated androstenedione-induced uterine hypertrophy in immature female rats with an ED50 of 0.03 mg/kg when given orally. In the same model, aminoglutethimide elicits the same effect with an ED50 of 30 mg/kg when given orally[1]. Fadrozole hydrochloride prevents the development of both benign and malignant spontaneus mammary neoplasns in female Sprague-Dawley rats. It also slows the spontaneous development of ptuitary pars dta mas in female rats, and reduces the of spontaneous hcu ar tumours in male and female rats[2]. Administration of fadrozole in male and female mice suppresses the production of 17b-estradiol, accompanied with a 70% reduction in parasite burden. This protective effect is associated in male mice with a recovery of the specific cellular immune response. Interleukin-6 (IL-6) serum levels, and its production by splenocytes, is augmented by 80%, together with a 10-fold increase in its expression in testes of infected male mice. Fadrozole treatment returns these levels to baseline values[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

223.27

Appearance

Solid

Formula

C14H13N3
CAS No.
SMILES

N#CC1=CC=C(C2CCCC3=CN=CN23)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (447.89 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.4789 mL 22.3944 mL 44.7888 mL
5 mM 0.8958 mL 4.4789 mL 8.9578 mL
10 mM 0.4479 mL 2.2394 mL 4.4789 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (9.72 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.17 mg/mL (9.72 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (9.72 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.69%

COA (246 KB) LCMS (91 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[2][3]

Rats: Rats are treated with daily dosing with fadrozole hydrochloride (CGS 16949A) in purified water by gavage for 2 years. There are 60 rats in each of four groups given 0, 0.05, 0.25 or 1.25 mg/kg daily. Control rats receive only water. Clinical signs are recorded weekly and the animals are examine for palpable masses every 4 weeks for the first 9 months, then every 2 weeks for the remainder of the study[2].

Mice: Fadrozole is administered in the form of sub-dermal long-term release pellets (20 mg/wt kg, in three-week-release pellets), starting 1 week prior to the infection, using a 10-gauge needle. Three pellets are administrated during the study. Placebo pellets are administered to another group of infected mice, in the same fashion as the inhibitor. After 1 week, mice are infected and killed 8 weeks later[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
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Keywords:

Fadrozole102676-47-1CGS 16949A (Rac)-FAD286Cytochrome P450CYPsInhibitorinhibitorinhibit

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